Understanding how drugs work in vivo is critical for drug design and for maximizing the potential of currently available drugs. 5-nitrofurans are a class of prodrugs widely used to treat bacterial and trypanosome infections, but despite relative specificity, 5-nitrofurans often cause serious toxic side effects in people. Here, we use yeast and zebrafish, as well as human in vitro systems, to as...

A series of novel N'-((5-nitrofuran-2-yl/4-nitrophenyl) methylene) substituted hydrazides (3a-3i & 4a-4i) was synthesized, and tested for in vitro antimycobacterial activity, and their quantitative structure activity relationship (QSAR) of hydrazide derivatives is reported here. The results of anti-mycobacterial activity study indicated that the presence of halogen substitution at benzohydrazid...

A series of (5-nitrofuran-2-yl)-1, 3, 4-thiadiazole-2-yl derivatives 6a-6e have been synthesized and screened for in-vitro anti-leishmanial activity against the promastigote form of L. major. The structure of Schiff bases were confirmed by 1H NMR, IR. Screening results indicate that all of the designed and synthesized final compounds (6a-6e) significantly reduced the viability of promastigotes ...

Three 5-nitrofuran derivatives showed carcinogenic activity when fed to female Holtzman rats at levels of 0.1 to 0.3% in a commercial diet for up to 44.5 weeks, while 2 other 5-nitrofuran derivatives and 5,5-diphenylhydantoin were inactive. Formic acid 2-[4-(5-nitro-2-furyl)-2-thiazolyl]hydrazide induced benign and malignant tumors of the mammary glands, adenomas or adenocarcinomas of the kidne...

The reductively activated nitroaromatic class of antimicrobials, which include nitroimidazole and the more metabolically labile nitrofuran antitubercular agents, have demonstrated some potential for development as therapeutics against dormant TB bacilli. In previous studies, the pharmacokinetic properties of nitrofuranyl isoxazolines were improved by incorporation of the outer ring elements of ...

A nitrofuran-containing medium, FTO agar, supported the growth of Micrococcus and prevented the growth of Staphylococcus. Its potential as a differential medium is considered worthy of clinical trial.

A complete stereocontrol of 1,3-dipolar cycloaddition of N-metalated azomethine ylides onto endohedral fullerene H2@C60 is reported for the first time. The stereodivergent synthesis of either the cis or the trans endohedral cycloadduct is achieved with excellent diastereo- and enantioselectivities.

Three antimicrobial nitroimidazole drugs (metronidazole, dimetridazole, and tinidazole) inhibit a range of clostridia and the protozoan Trichomonas vaginalis ; they have an identical site and mode of action as specific electron acceptors from the pyruvate phosphoroclastic reaction. Analogues of the drugs are compared and the structural requirements for activity explained. The nitrofuran (nitrof...